AMG-47A |
| Katalog-Nr.GC17669 |
AMG-47a ist ein potenter und oral aktiver Lymphozyten-spezifischer Protein-Tyrosin-Kinase (Lck)-Inhibitor mit einem IC50 von 0,2 nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 882663-88-9
Sample solution is provided at 25 µL, 10mM.
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AMG-47A is a destabilizer of the KRAS oncoprotein.
Ras is a small GTPase that involves in numerous cellular signaling pathways governing growth, survival, and motility. In humans, there are three Ras genes: KRAS, HRAS, and NRAS. Oncogenic
mutations in all three Ras family members have been identified in human cancers. In particular, KRAS is one of the most frequently mutated oncogenes across cancer types.[1]
In the HeLa EGFP-KRASG12V cells, 48-hour treatment of AMG-47a has a 30–40% decrease in EGFP signal, treating cells for 3 and 5 days shows the similar results. AMG-47a selectively affects EGFP-KRASG12V protein levels. AMG-47a also has a mild effect on EGFP-KRASG12V protein levels after three days. The loss of EGFP-KRASG12V signal plateaus at 50% for AMG-47a. [1]
References:
1. Carver J, Dexheimer TS, Hsu D et al. A high-throughput assay for small molecule destabilizers of the KRASoncoprotein. PLoS One. 2014 Aug 5;9(8):e103836
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